In rodents, 8β-VE2 stimulates follicular growth and to a comparable extent as estradiol, whereas the highly ERα-selective agonist 16α-LE2 has no effect on ovarian follicle development, indicating that the ERβ and not the ERα is involved in the effects of estrogen on ovarian follicles.[2][3] In contrast, 16α-LE2 stimulates uterine weight, whereas 8β-VE2 has no effect, indicating that the ERα and not the ERβ is involved in the effects of estrogen on the uterus.[2]
Research has determined through experimental rodent studies with estradiol, 16α-LE2, and 8β-VE2 that the positive, protective effects of estrogens on bone formationresorption and bone mineral density are mediated via the ERα, whereas the ERβ does not appear to be involved.[4] On the other hand, while both ERα and ERβ are expressed in skeletal muscle, it was found that ERβ is the predominant ER subtype that is responsible for estrogen stimulation of skeletal muscle growth and regeneration.[5] Moreover, similarly to testosterone, 8β-VE2 has anabolic effects in skeletal muscle and significantly increases muscle mass as well as produces muscle hypertrophy in rats.[5] In contrast to testosterone however, 8β-VE2 shows no androgenic effects.[5] The effects of 8β-VE2 and ERβ may be mediated, in part, by local stimulation of insulin-like growth factor 1 (IGF-1)-induced myogenicprotein synthesis, as 8β-VE2 has been found to strongly induce expression of IGF-1 in the rat levator ani muscle.[5]
^ abPakdel F, Kah O, Jégou B (31 March 2009). "Mechanisms of action of particular endocrine-disrupting chemicals". In Shaw I (ed.). Endocrine-Disrupting Chemicals in Food. Elsevier. pp. 550–. ISBN978-1-84569-574-3.
^ abcdeHegele-Hartung C, Siebel P, Peters O, Kosemund D, Müller G, Hillisch A, et al. (April 2004). "Impact of isotype-selective estrogen receptor agonists on ovarian function". Proceedings of the National Academy of Sciences of the United States of America. 101 (14): 5129–5134. Bibcode:2004PNAS..101.5129H. doi:10.1073/pnas.0306720101. PMC387385. PMID 15037755.
^Binder K, Winuthayanon W, Hewitt SC, Couse JF, Korach KS (15 November 2014). "Steroid Receptors in the Uterus and Ovary". In Plant TM, Zeleznik AJ (eds.). Knobil and Neill's Physiology of Reproduction. Academic Press. pp. 1150–. ISBN978-0-12-397769-4.
^Hertrampf T, Schleipen B, Velders M, Laudenbach U, Fritzemeier KH, Diel P (September 2008). "Estrogen receptor subtype-specific effects on markers of bone homeostasis" (PDF). Molecular and Cellular Endocrinology. 291 (1–2): 104–108. doi:10.1016/j.mce.2008.03.003. PMID 18433985. S2CID 1774519.
^ abcdVelders M, Schleipen B, Fritzemeier KH, Zierau O, Diel P (May 2012). "Selective estrogen receptor-β activation stimulates skeletal muscle growth and regeneration". FASEB Journal. 26 (5): 1909–1920. doi:10.1096/fj.11-194779. PMID 22278942. S2CID 39692168.
February 15, 2024
vinylestradiol, also, known, vinylestra, triene, 17β, diol, synthetic, estrogen, featuring, estradiol, core, highly, potent, selective, agonist, erβ, that, used, scientific, research, study, function, erβ, fold, higher, potency, transactivation, assays, erβ, r. 8b VE2 or 8b vinylestradiol also known as 8b vinylestra 1 3 5 10 triene 3b 17b diol is a synthetic estrogen featuring an estradiol core 1 2 It is a highly potent and selective agonist of the ERb that is used in scientific research to study the function of the ERb 1 2 It has 190 fold higher potency in transactivation assays of the ERb relative to the ERa and 93 rat and 180 fold human preference in binding affinity for the ERb over the ERa 2 8b VE2Clinical dataOther names8b Vinylestradiol 8b Vinylestra 1 3 5 10 triene 3b 17b diolIdentifiersIUPAC name 8b Vinylestra 1 3 5 10 triene 3 17b diolCAS Number367929 02 0 YChemSpider8007830UNIID5KU4JGS7YChemical and physical dataFormulaC 20H 26O 2Molar mass298 426 g mol 13D model JSmol Interactive imageSMILES C C C 12CCC3 CC O CC C3 C 1 H CC C 4 C 2 H CC C 4 H O CInChI InChI 1S C20H26O2 c1 3 20 11 8 13 12 14 21 4 5 15 13 16 20 9 10 19 2 17 20 6 7 18 19 22 h3 5 12 16 18 21 22H 1 6 11H2 2H3 t16 17 18 19 20 m1 s1Key NMCRWZRLOOYKTG SWBPCFCJSA NIn rodents 8b VE2 stimulates follicular growth and to a comparable extent as estradiol whereas the highly ERa selective agonist 16a LE2 has no effect on ovarian follicle development indicating that the ERb and not the ERa is involved in the effects of estrogen on ovarian follicles 2 3 In contrast 16a LE2 stimulates uterine weight whereas 8b VE2 has no effect indicating that the ERa and not the ERb is involved in the effects of estrogen on the uterus 2 Research has determined through experimental rodent studies with estradiol 16a LE2 and 8b VE2 that the positive protective effects of estrogens on bone formation resorption and bone mineral density are mediated via the ERa whereas the ERb does not appear to be involved 4 On the other hand while both ERa and ERb are expressed in skeletal muscle it was found that ERb is the predominant ER subtype that is responsible for estrogen stimulation of skeletal muscle growth and regeneration 5 Moreover similarly to testosterone 8b VE2 has anabolic effects in skeletal muscle and significantly increases muscle mass as well as produces muscle hypertrophy in rats 5 In contrast to testosterone however 8b VE2 shows no androgenic effects 5 The effects of 8b VE2 and ERb may be mediated in part by local stimulation of insulin like growth factor 1 IGF 1 induced myogenic protein synthesis as 8b VE2 has been found to strongly induce expression of IGF 1 in the rat levator ani muscle 5 See also editDiarylpropionitrile ERB 196 Erteberel FERb 033 Prinaberel WAY 166818 WAY 200070 WAY 214156References edit a b Pakdel F Kah O Jegou B 31 March 2009 Mechanisms of action of particular endocrine disrupting chemicals In Shaw I ed Endocrine Disrupting Chemicals in Food Elsevier pp 550 ISBN 978 1 84569 574 3 a b c d e Hegele Hartung C Siebel P Peters O Kosemund D Muller G Hillisch A et al April 2004 Impact of isotype selective estrogen receptor agonists on ovarian function Proceedings of the National Academy of Sciences of the United States of America 101 14 5129 5134 Bibcode 2004PNAS 101 5129H doi 10 1073 pnas 0306720101 PMC 387385 PMID 15037755 Binder K Winuthayanon W Hewitt SC Couse JF Korach KS 15 November 2014 Steroid Receptors in the Uterus and Ovary In Plant TM Zeleznik AJ eds Knobil and Neill s Physiology of Reproduction Academic Press pp 1150 ISBN 978 0 12 397769 4 Hertrampf T Schleipen B Velders M Laudenbach U Fritzemeier KH Diel P September 2008 Estrogen receptor subtype specific effects on markers of bone homeostasis PDF Molecular and Cellular Endocrinology 291 1 2 104 108 doi 10 1016 j mce 2008 03 003 PMID 18433985 S2CID 1774519 a b c d Velders M Schleipen B Fritzemeier KH Zierau O Diel P May 2012 Selective estrogen receptor b activation stimulates skeletal muscle growth and regeneration FASEB Journal 26 5 1909 1920 doi 10 1096 fj 11 194779 PMID 22278942 S2CID 39692168 Retrieved from https en wikipedia org w index php title 8b VE2 amp oldid 1191899070, wikipedia, wiki, book, books, library,
